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    • 1. 发明授权
    • Process for preparation of glycidyl ether
    • 缩水甘油醚的制备方法
    • US5359097A
    • 1994-10-25
    • US571543
    • 1990-08-22
    • Kiyoshi KawamuraTomio Ota
    • Kiyoshi KawamuraTomio Ota
    • C07D301/28C07D303/22C07D405/12C07D407/12C07D417/12C07D311/04
    • C07D303/22C07D407/12
    • A process is provided for preparation of a glycidyl ether represented by the general formula ##STR1## wherein A represents an aryl group optionally having a substituent or a heteroaryl group optionally having a substituent, and the carbon atom marked with * is an asymmetric carbon,which comprises reacting an aryl alcohol represented by the general formulaA--OH (I)wherein A is as defined above,with an epihalohydrin in the presence of a quaternary ammonium salt; and, if necessary, further treating the reaction product with a base. According to the present process, it is possible to prepare by simple procedures and in a high optical purity glycidyl ethers of the above formula (II) useful as an intermediate for preparation of medicines, particularly medicines having .beta.-adrenoreceptor blocking action or the like.
    • PCT No.PCT / JP89 / 01293 Sec。 371 1990年7月18日第 102(e)日期1990年7月18日PCT提交1989年12月25日PCT公布。 出版物WO90 / 07506 日本1990年7月12日提供了一种制备由任选具有取代基的通式或由任选具有取代基的杂芳基表示的缩水甘油醚的方法,标有*的碳原子是不对称碳,其包括使 由季铵盐存在下的表卤代醇,由通式A-OH(I)表示的芳基醇,其中A如上所定义; 并且如果需要,用碱进一步处理反应产物。 根据本方法,可以通过简单的方法和上述式(II)的高光学纯度的缩水甘油醚制备,其可用作制备药物的中间体,特别是具有β-肾上腺素受体阻断作用的药物等。
    • 4. 发明授权
    • Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity
    • 具有5-HT 4受体激动活性的喹诺酮羧酸化合物
    • US07964727B2
    • 2011-06-21
    • US10595948
    • 2004-11-10
    • Tomoki KatoKiyoshi KawamuraMikio MoritaChikara Uchida
    • Tomoki KatoKiyoshi KawamuraMikio MoritaChikara Uchida
    • C07D221/02C07D215/00C07D413/00A01N43/40A01N43/42A61K31/435A61K31/44
    • C04B35/632C07D401/12C07D401/14C07D405/14
    • This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
    • 本发明提供式(I)化合物:其中Het表示具有一个氮原子的杂环基团,B直接与该碳原子结合,并且具有4至7个碳原子,所述杂环基团未被取代或被1至4个取代基取代 独立地选自取代基α1; A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R1表示异丙基,正丙基或环戊基; R2表示甲基,氟原子或氯原子; R3独立地表示(i)氧代基,羟基,氨基,烷基氨基或羧基; (ii)具有3至8个碳原子的环烷基,所述环烷基被1至5个取代基取代,或(iii)具有3至8个原子的杂环基,所述杂环基未被取代或被1 至5个取代基,n为1,2或3,或其药学上可接受的盐。 这些化合物具有5-HT 4受体激动活性,因此可用于治疗哺乳动物特别是人类的胃食管反流病,非溃疡性消化不良,功能性消化不良,肠易激综合征等。
    • 5. 发明授权
    • Polymer, crosslinked polymer, composition for solid polymer electrolyte, solid polymer electrolyte, and adhesive composition
    • 聚合物,交联聚合物,固体聚合物电解质的组合物,固体聚合物电解质和粘合剂组合物
    • US07645830B2
    • 2010-01-12
    • US11795783
    • 2006-01-18
    • Takeshi NiitaniMasato AmaikeMikiya ShimadaKiyoshi Kawamura
    • Takeshi NiitaniMasato AmaikeMikiya ShimadaKiyoshi Kawamura
    • C08F118/02C08L31/02C09J167/06
    • C08F293/005C08F290/06C08F293/00C08F297/02C08F297/026C08G18/6229C08L25/04C08L27/16C08L29/02C08L53/00C08L71/02C08L75/04C08L2205/05C08L2666/02C09J153/00H01M10/052H01M10/0565H01M2300/0082C08L2666/04
    • A polymer including a block chain A which is formed from a random copolymer containing a repeating unit (I) represented by the formula (I) wherein R1 to R3 each independently represents hydrogen or C1-10 hydrocarbon and R1 and R3 may bond to form a ring; R4a and R4b each independently represents hydrogen or methyl; R5 represents hydrogen, hydrocarbon, acyl, or silyl; and m represents any integer of 1 to 100 and when m is 2 or more and each R4a may be the same or different from one another and each R4b may be the same or different from one another; and a repeating unit (II) represented by the formula (II) wherein R6 and R8 each independently represents hydrogen or C1-10 hydrocarbon and R6 and R8 may bond to form a ring; R7 represents hydrogen, C1-10 hydrocarbon, hydroxyl, hydrocarbonoxy, carboxyl, acid anhydride, amino, ester, or an organic group having at least one functional group selected from the group consisting of hydroxyl, carboxyl, epoxy, acid anhydride, and amino; and R9 represents an organic group having at least one functional group selected from the group consisting of hydroxyl, carboxyl, epoxy, acid anhydride, and amino; and a block chain B having a repeating unit (III) represented by the formula (III) wherein R10 to R12 each independently represents hydrogen or C1-10 hydrocarbon and R13 represents aryl or heteroaryl; and wherein an arrangement order thereof is B, A, B.
    • 一种包含嵌段链A的聚合物,其由含有式(I)表示的重复单元(I)的无规共聚物形成,其中R 1至R 3各自独立地表示氢或C 1-10烃,并且R 1和R 3可以键合形成 环; R4a和R4b各自独立地表示氢或甲基; R5表示氢,烃,酰基或甲硅烷基; m表示1〜100的整数,m为2以上时,各R​​ 4a可以相同也可以不同,各R 4a可以相同也可以不同。 和由式(II)表示的重复单元(II),其中R6和R8各自独立地表示氢或C1-10烃,R6和R8可以键合形成环; R7表示氢,C1-10烃,羟基,烃氧基,羧基,酸酐,氨基,酯或具有至少一个选自羟基,羧基,环氧基,酸酐和氨基的官能团的有机基团; 并且R 9表示具有至少一个选自羟基,羧基,环氧基,酸酐和氨基的官能团的有机基团; 和具有由式(III)表示的重复单元(III)的嵌段链B,其中R10至R12各自独立地表示氢或C1-10烃,R13表示芳基或杂芳基; 其布置顺序为B,A,B。
    • 6. 发明授权
    • Oxyindole derivatives
    • 氧吲哚衍生物
    • US07589109B2
    • 2009-09-15
    • US11360095
    • 2006-02-22
    • Chikara UchidaHiroki SoneKiyoshi Kawamura
    • Chikara UchidaHiroki SoneKiyoshi Kawamura
    • A61K31/454C07D403/14
    • C07D401/12C07D401/14C07D405/14
    • This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R1, R2, R3, R4 and R5 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
    • 本发明涉及式(I)化合物或其药学上可接受的盐,其中:A,R 1,R 2,R 3,R 4和R 5各自如本文所述或其药学上可接受的盐,以及含有这些化合物的组合物和 使用这些化合物治疗由5-HT4激动活性介导的病症,例如但不限于胃食道反流病,胃肠道疾病,胃动力障碍,非溃疡性消化不良,功能性消化不良,肠易激综合征(IBS) ),便秘,消化不良,食道炎,胃食管疾病,恶心,中枢神经系统疾病,阿尔茨海默病,认知障碍,呕吐,偏头痛,神经系统疾病,疼痛,心血管疾病,心力衰竭,心律失常,糖尿病或呼吸暂停综合征。